ASP7663

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ASP7663 是一种 TRPA1 受体激动剂，在体内表现出腹部镇痛作用。

ASP7663 is a?TRPA1 Receptor Agonist?and exhibiting an abdominal analgesic effect in vivo.?

ASP7663 concentration dependently increases intracellular Ca2+ concentration in human, rat, and mouse TRPA1 expressed in HEK293 cells in a similar manner, with respective EC50 values (95% confidence interval [CI]) of 0.51 (0.40–0.66), 0.54 (0.41–0.72), and 0.50 (0.41–0.63) μmol/L.ASP7663 concentration-dependently stimulates 5-HT release from QGP-1 cells, a lineage of TRPA1-expressing EC cells, with an EC50 value of 72.5 (52.6–99.9) μmol/L.

ASP7663 significantly improves the loperamide-induced delay in colonic transit in mice. ASP7663 (orally, 0.3 and 1 mg/kg) significantly shortens the prolonged bead expulsion time caused by loperamide.ASP7663 (orally, 1 and 3 mg/kg) exhibits inhibitory effects on colorectal distension in rat. Animal Model:CRD model (colorectal distension in rat).Dosage:1 and 3 mg/kg.Administration:Orally.Result:Significantly reduced the number of abdominal contractions evoked during CRD at pressures of 30, 45, and 60 mmHg. ASP7663 also reduced the number of abdominal contractions by intravenous treatment.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPA1

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1190217-35-6

263.26

C14H14FNO3?

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (189.93 mM)

CC(C)CN1C(=O)\C(=C\C(O)=O)c2cccc(F)c12

(2E)-2-[7-Fluoro-12-dihydro-1-(2-methylpropyl)-2-oxo-3H-indol-3-ylidene]acetic acid

(-20℃)

With Ice Pack

≥ 2 years